DEPOT FORMULATIONS
Pharmaceutical compositions comprising an active pharmaceutical ingredient, a high viscosity liquid carrier material, a hydrophobic solvent, and a hydrophilic solvent are disclosed. Also disclosed are methods of manufacturing and using the compositions. The compositions are suitable for use, e.g., as depot formulations.
1 . A composition comprising:
sirolimus present in an amount ranging from about 1 wt % to about 5 wt %, based on weight of the composition;
sucrose acetate isobutyrate (SAIB) present in an amount ranging from about 0.5 wt % to about 5 wt %, based on weight of the composition;
benzyl benzoate present in an amount ranging from about 35 wt % to about 50 wt %, based on weight of the composition;
ethanol present in an amount ranging from about 1 wt % to about 10 wt %, based on weight of the composition;
polyethylene glycol (PEG) present in an amount ranging from about 40 wt % to about 50 wt %, based on weight of the composition; and
vitamin E in an amount ranging from about 0.01 wt % to about 5 wt %.
2 .- 9 . (canceled)
10 . The composition of claim 1 , wherein the benzyl benzoate is present in an amount ranging from about 35 wt % to about 45 wt %, based on weight of the composition.
11 .- 15 . (canceled)
16 . The composition of claim 1 , wherein the ethanol is present in an amount ranging from about 1 wt % to about 7 wt %, based on weight of the composition.
17 .- 24 . (canceled)
25 . The composition of claim 1 , wherein the vitamin E is present in an amount ranging from about 0.1 wt % to about 5 wt %, based on weight of the composition.
26 . The composition of claim 1 , wherein the vitamin E is present in an amount ranging from about 0.5 wt % to about 2 wt %, based on weight of the composition.
27 . The composition of claim 1 , wherein the composition has a weight ratio of SAIB:vitamin E ranging from about 0.5 to about 10.
28 .- 29 . (canceled)
30 . The composition of claim 1 , the composition consisting essentially of:
sirolimus in an amount ranging from about 1 wt % to about 5 wt %, based on weight of the composition;
SAIB in an amount ranging from about 0.1 wt % to about 10 wt %, based on weight of the composition;
benzyl benzoate in an amount ranging from about 30 wt % to about 45 wt %, based on weight of the composition;
ethanol in an amount ranging from about 1 wt % to about 10 wt %, based on weight of the composition;
PEG400 in an amount ranging from about 40 wt % to about 50 wt %, based on weight of the composition; and
vitamin E in an amount ranging from about 0.5 wt % to about 2 wt %, based on weight of the composition.
31 .- 33 . (canceled)
34 . The composition of claim 1 , wherein the composition is pharmaceutically acceptable.
35 . A method of treating a subject afflicted with an eye condition, the method comprising:
administering a composition to an eye of a subject in need thereof, wherein the composition comprises an effective amount of an active pharmaceutical ingredient capable of treating the eye condition, the composition comprising:
an active pharmaceutical ingredient;
a high viscosity liquid carrier material (HVLCM);
a first hydrophobic solvent; and
a hydrophilic solvent.
36 . (canceled)
37 . The method of claim 35 , wherein the eye condition comprises uveitis, diabetic macular edema, or wet age-related macular degeneration.
38 . The method of claim 35 , wherein the administering comprises injecting.
39 . The composition of claim 1 , wherein the benzyl benzoate is present in an amount ranging from about 40 wt % to about 50 wt %, based on weight of the composition.
40 . The composition of claim 1 , wherein the ethanol is present in an amount ranging from about 3 wt % to about 10 wt %, based on weight of the composition.
41 . The composition of claim 1 , wherein a weight ratio of SAIB to vitamin E ranges from about 60:1 to about 1:2.
42 . The composition of claim 1 , wherein a weight ratio of SAIB to vitamin E ranges from about 10:1 to about 1:1.8.
43 . The composition of claim 1 , wherein a weight ratio of SAIB to vitamin E ranges from about 5:1 to about 1:1.5.
44 . The composition of claim 1 , wherein a weight ratio of SAIB to vitamin E ranges from about 2:1 to about 1:1.5.
45 . The composition of claim 1 , wherein the composition has a density at 25° C. and 1 atmosphere ranging from 1.02 g/mL to 1.15 g/mL.
46 . The composition of claim 1 , wherein the composition has a viscosity ranging from about 1 cP to about 150 cP at 25° C. and 1 atmosphere.
47 . The composition of claim 1 , wherein the vitamin E is present in an amount ranging from about 0.02 wt % to about 0.09 wt %, based on weight of the composition.